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Ethimizol, 4,5-di(methylcarbamoyl)-1-ethyl-imidazole, was metabolized into at least six metabolites in an isolated perfused rat liver preparation. Based on TLC and mass spectrometry, 4-carbamoyl-5-methylcarbamoyl-1-ethyl-imidazole and 4,5-di(methylcarbamoyl)-imidazole were identified as the primary metabolites of ethimizol. These undergo further… (More)
The once-through perfused (18 ml/min) rat liver preparations from vehicle-, phenobarbital (PB)-, and 3-methylcholanthrene (3-MC)-treated rats were used for the study of 14C-ethimizol [4,5-di(methylcarbamoyl)-1-ethyl-imidazole] elimination after input concentrations of 5, 25, 50, and 100 microM. The steady state hepatic extraction ratios decreased with… (More)
It is shown for the first time that the mammalian enzymes can cause the degradation of the C60 fullerene molecules. This biodegradation is caused by the action of а hypochlorite generated neutrophil enzyme myeloperoxidase of fullerene molecule and leads to the loss of the topology of the fullerene core.
The present report describes development of hexamethonium complexes based on fullerene C60. Hexamethonium has a limited penetration into CNS and therefore can antagonize central effects of nicotine only when given at high doses. In the present studies conducted in laboratory rodents, intraperitoneal administration of hexamethonium-fullerene complexes… (More)